Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 456778Generated: October 27, 2026

Hydrochloric Acid → Asp-4000

https://huagongshe.com/reaction/456778

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHydrochloric AcidHCID 313—
Reactanttert-Butyl (1R,3S,4S,6R)-3-{[(2S)-2-cyano-1-pyrrolidinyl]carbonyl}-6-hydroxy-2-azabicyclo[2.2.1]heptane-2-carboxylateHCID 86598896—
SolventWaterHCID 962—
Solvent1,4-DioxaneHCID 31275—
ProductAsp-4000HCID 24905398—

Reaction Steps

To a solid of tert-butyl (1R,3S,4S,6R)-3-{[(2S)-2-cyano-1-pyrrolidinyl]carbonyl}-6-hydroxy-2-azabicyclo[2.2.1]heptane-2-carboxylate obtained in Example 42-8 (796 mg), was added a mixture of 4N hydrochloride in dioxane (1.87 mL) and water (0.13 mL). The mixture was stirred at room temperature for 5 minutes. The resulting mixture was evaporated in vacuo and the residual solid was washed with isopropyl alcohol. The solid was recrystalized from ethanol-water to give the target compound as a white crystal (367 mg)

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07186731B2
Source datasetuspto-grants-2007_03
ORD IDord-94894c4656a44bbe9e3970e8c317bb4e
Source noteuspto-grants-2007_03